货号	规格	价格	上海	北京	珠海	重庆	武汉
S80890-2mg买3赠1	99.10%	￥200.00 S80890-2mg ￥200.00 现货（买3赠1）	5 5	-	-	-	-
S80890-5mg促销	99.10%	￥320.00 ￥256.00 S80890-5mg ￥256.00 现货	4 4	-	-	-	-
S80890-10mg促销	99.10%	￥490.00 ￥392.00 S80890-10mg ￥392.00 现货	6 6	-	-	-	-
S80890-25mg促销	99.10%	￥690.00 ￥620.00 S80890-25mg ￥620.00 现货	3 3	-	-	-	-
S80890-50mg	≥99%	￥1110.00 S80890-50mg ￥1110.00 2-3天	0 货期：2-3天	-	-	-	-
S80890-100mg	≥99%	￥1780.00 S80890-100mg ￥1780.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.

靶点：

p110α:11 nM (IC50);p110γ:18 nM (IC50);p110δ:58 nM (IC50);p110β:350 nM (IC50);hsVPS34:830 nM (IC50);PI3KC2β:64 nM (IC50);PI3KC2α:47 nM (IC50);DNA-PK:13 nM (IC50);ATM:610 nM (IC50);PI4KIIIα:830 nM (IC50);PI4KIIIβ:3.1 μM (IC50);mTORC1:1.05 μM (IC50);ATR:15 μM (IC50);DNA-PK;PI3K

体内研究：

To test the efficacy of Roscovitine and PIK-90 in vivo, GBM43 cells are implanted s.c. into nude mice. Mice with established tumors are randomized into four treatment groups: vehicle (PBS:H2O), Roscovitine, PIK-90, or PIK-90 plus Roscovitine. After 12 d of treatment, both Roscovitine and PIK-90 show clear single-agent efficacy, with tumor size in mice treated with Roscovitine and PIK-90 in combination significantly smaller than either vehicle or monotherapy-treated controls. Roscovitine is less effective than PIK-90 in blocking proliferation (levels of Ki-67), whereas combination therapy shows essentially additive antiproliferative effects

参考文献：

1. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. 2. Niedermeier M, et al. Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach. Blood. 2009 May 28;113(22):5549-57. 3. Cheng CK, et al. Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12722-7.

溶解性：

DMSO : 6.67 mg/mL (18.98 mM; ultrasonic and adjust pH to 2 with HCl)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.846 ml	14.23 ml	28.461 ml
5 mM	0.569 ml	2.846 ml	5.692 ml
10 mM	0.285 ml	1.423 ml	2.846 ml
50 mM	0.057 ml	0.285 ml	0.569 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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